DK73594A - Fremgangsmåde til fremstilling af 17-substituerede 4-aza-5,7-androstadien-3-on-derivater - Google Patents

Fremgangsmåde til fremstilling af 17-substituerede 4-aza-5,7-androstadien-3-on-derivater

Info

Publication number
DK73594A
DK73594A DK073594A DK73594A DK73594A DK 73594 A DK73594 A DK 73594A DK 073594 A DK073594 A DK 073594A DK 73594 A DK73594 A DK 73594A DK 73594 A DK73594 A DK 73594A
Authority
DK
Denmark
Prior art keywords
aza
substituted
preparation
androstadien
derivatives
Prior art date
Application number
DK073594A
Other languages
English (en)
Other versions
DK169840B1 (da
Inventor
Dennis Alan Holt
Mark Alan Levy
Brian Walter Metcalf
Original Assignee
Smithkline Beckman Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Smithkline Beckman Corp filed Critical Smithkline Beckman Corp
Publication of DK73594A publication Critical patent/DK73594A/da
Application granted granted Critical
Publication of DK169840B1 publication Critical patent/DK169840B1/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/003—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring the S atom directly linked to a ring carbon atom of the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
DK073594A 1987-01-28 1994-06-21 Fremgangsmåde til fremstilling af 17-substituerede 4-aza-5,7-androstadien-3-on-derivater DK169840B1 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/007,539 US4888336A (en) 1987-01-28 1987-01-28 Steroid 5-alpha-reductase inhibitors
US753987 1987-01-28

Publications (2)

Publication Number Publication Date
DK73594A true DK73594A (da) 1994-06-21
DK169840B1 DK169840B1 (da) 1995-03-13

Family

ID=21726780

Family Applications (4)

Application Number Title Priority Date Filing Date
DK037388D DK168525B1 (da) 1987-01-28 1988-01-26 17-substituerede 4-aza-5-alfa-androsten-3-on-derivater samt farmaceutisk middel med indhold deraf
DK037388A DK37388A (da) 1987-01-28 1988-01-26 Steroid-5-alfa-reduktaseinhibitorer
DK196691A DK169438B1 (da) 1987-01-28 1991-12-05 Fremgangsmåde til fremstilling af 17 substituerede 4-aza-5alfa-androsten-3-on-derivater samt mellemprodukter til anvendelse ved fremgangsmåden
DK073594A DK169840B1 (da) 1987-01-28 1994-06-21 Fremgangsmåde til fremstilling af 17-substituerede 4-aza-5,7-androstadien-3-on-derivater

Family Applications Before (3)

Application Number Title Priority Date Filing Date
DK037388D DK168525B1 (da) 1987-01-28 1988-01-26 17-substituerede 4-aza-5-alfa-androsten-3-on-derivater samt farmaceutisk middel med indhold deraf
DK037388A DK37388A (da) 1987-01-28 1988-01-26 Steroid-5-alfa-reduktaseinhibitorer
DK196691A DK169438B1 (da) 1987-01-28 1991-12-05 Fremgangsmåde til fremstilling af 17 substituerede 4-aza-5alfa-androsten-3-on-derivater samt mellemprodukter til anvendelse ved fremgangsmåden

Country Status (13)

Country Link
US (1) US4888336A (da)
EP (1) EP0277002B1 (da)
JP (1) JPS63192800A (da)
AT (1) ATE77388T1 (da)
AU (1) AU608560B2 (da)
CA (1) CA1325006C (da)
DE (1) DE3871965T2 (da)
DK (4) DK168525B1 (da)
ES (1) ES2042725T3 (da)
GR (1) GR3005284T3 (da)
IE (1) IE61594B1 (da)
PT (1) PT86652B (da)
ZA (1) ZA88549B (da)

Families Citing this family (53)

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US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
US4814324A (en) * 1987-03-06 1989-03-21 Merck & Co., Inc. Sterol inhibitors of testosterone 5α-reductase
US5595985A (en) * 1989-03-10 1997-01-21 Endorecherche Inc. Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia
US5372996A (en) * 1989-03-10 1994-12-13 Endorecherche, Inc. Method of treatment of androgen-related diseases
US5405978A (en) * 1989-05-30 1995-04-11 The Upjohn Company Oxidative preparation of 3,5-secoandrost-5-one-3,17 β-dioic acid
EP0943328B1 (en) * 1989-07-07 2004-06-16 Endorecherche Inc. Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia
AU5856090A (en) * 1989-07-07 1991-02-06 Endorecherche Inc. Androgen derivatives for use in the inhibition of sex steroid activity
ES2189784T3 (es) * 1989-07-07 2003-07-16 Endorech Inc Procedimiento para el tratamiento de enfermedades relacionadas con adrogenos.
US5098908A (en) * 1990-06-20 1992-03-24 Merck & Co., Inc. 17β-hydroxybenzoyl-4-aza-5α-androst-1-en-3-ones as testosterone reductase inhibitors
US5151430A (en) * 1990-06-20 1992-09-29 Merck & Co., Inc. Specific 17β-thiobenzoyl-4-aza-5α-androst-1-en-3-ones as antiandrogen agents
US5162332A (en) * 1990-06-20 1992-11-10 Merck & Co., Inc. Selected 17 β-polyaroyl-4-aza-5 α-androst-1-en-3-ones as steroidal reductase inhibitors
US5061802A (en) * 1990-06-20 1991-10-29 Merck & Co. Inc. 17β-aminobenzoyl-4-aza-5α-androst-1-en-3-ones as benign prostatic hypertrophy agents
US5091380A (en) * 1990-06-28 1992-02-25 Merck & Co., Inc. N-monosubstituted adamantyl/norbornanyl 17β-carbamides of 3-carboxy-androst-3,5-dienes as testosterone 5α-reductase inhibitors
NZ241979A (en) * 1991-03-20 1996-01-26 Merck & Co Inc Treatment of benign prostatic hyperplasia using 5alpha-reductase inhibitor and an alpha1-adrenergic recepter blocker
US5250539A (en) * 1991-08-21 1993-10-05 Eli Lilly And Company Hexahydrobenzo[f]quinolinones
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
CA2084799C (en) 1991-12-17 2003-01-28 Glenn J. Gormley Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones
EP0547687A1 (en) * 1991-12-18 1993-06-23 Merck & Co. Inc. 17B-N-Substituted adamantyl/norbonanyl carbamoyl-4-aza-5a-and-rost-1-en-3-ones and androstan-3 ones
EP0641356B1 (en) * 1991-12-20 1998-04-22 Glaxo Wellcome Inc. Inhibitors of 5-alpha-testosterone reductase
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
WO1993023038A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
EP0641209A4 (en) * 1992-05-20 1995-08-23 Merck & Co Inc NEW 17-ESTER, AMID AND KETONE DERIVATIVES OF 3-OXO-4-AZASTEROIDS AS 5-ALPHA REDUCTINE INHIBITORS.
US5510351A (en) * 1992-05-20 1996-04-23 Merck & Co., Inc. Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
CA2135173A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel Ester derivatives of 4-aza-steroids
HUT71484A (en) * 1992-05-20 1995-11-28 Merck & Co Inc Process for producing of 7beta-substituted-4-aza-5alpha-cholestan-ones as 5-alpha-reductase inhibitors and pharmaceuticals compositions containing them
AU668180B2 (en) * 1992-05-20 1996-04-26 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
AU672978B2 (en) * 1992-05-20 1996-10-24 Merck & Co., Inc. 4-azasteroid 5-alpha-reductase inhibitors
AU680818B2 (en) * 1992-05-21 1997-08-14 Endorecherche Inc. Improved antiandrogens
GB9210880D0 (en) * 1992-05-21 1992-07-08 Smithkline Beecham Corp Compounds
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン５α−レダクターゼ活性の阻害剤
GB9213901D0 (en) * 1992-06-30 1992-08-12 Smithkline Beecham Corp Compounds
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
US5324734A (en) * 1992-09-15 1994-06-28 Merck & Co., Inc. Oxidization metabolites of 5-α-23-methyl-4-aza-21-nor-chol-1-ene-3, 20-dione
HU212459B (en) * 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
US5278159A (en) * 1992-10-06 1994-01-11 Merck & Co., Inc. Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
WO1994021614A1 (en) * 1993-03-24 1994-09-29 Merck & Co., Inc. SUBSTITUTED 3-PHENANTHRIDINONE DERIVATIVES AS 5α-REDUCTASE INHIBITORS
AU679769B2 (en) * 1993-06-28 1997-07-10 Merck & Co., Inc. 4-AZA-pregnane 5alpha-reductase isozyme 1 inhibitors
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5595996A (en) * 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
US6365597B1 (en) * 1996-02-14 2002-04-02 Aventis Pharmaceuticals Inc. 4-aza steroids
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
ATE473759T1 (de) 1998-05-22 2010-07-15 Univ Leland Stanford Junior Bifunktionelle moleküle sowie darauf basierende therapien.
CN102379684B (zh) 2005-04-28 2014-11-19 普罗透斯数字保健公司 药物信息系统
US9062126B2 (en) 2005-09-16 2015-06-23 Raptor Pharmaceuticals Inc. Compositions comprising receptor-associated protein (RAP) variants specific for CR-containing proteins and uses thereof
EP2398500B1 (en) 2009-02-20 2019-03-13 2-BBB Medicines B.V. Glutathione-based drug delivery system
ES2942923T3 (es) 2009-05-06 2023-06-07 Laboratory Skin Care Inc Composiciones de administración dérmica que comprenden complejos de agente activo-partículas de fosfato de calcio y métodos de uso de las mismas

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Publication number Priority date Publication date Assignee Title
US2897202A (en) * 1956-03-19 1959-07-28 Monsanto Chemicals 3-keto-4-aza-delta5-steroids and method of preparing same
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
KR830000085B1 (ko) * 1978-04-13 1983-02-08 제임스 에프. 너우톤 5α-환원효소 억제제로서 유용한 4-아자-17-치환-5α-안드로스탄-3-온류의 제조방법
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4220775A (en) * 1979-03-15 1980-09-02 Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors

Also Published As

Publication number Publication date
EP0277002A3 (en) 1988-10-26
CA1325006C (en) 1993-12-07
EP0277002B1 (en) 1992-06-17
DK168525B1 (da) 1994-04-11
DK196691D0 (da) 1991-12-05
AU608560B2 (en) 1991-04-11
IE880189L (en) 1988-07-28
PT86652B (pt) 1992-02-28
US4888336A (en) 1989-12-19
AU1077888A (en) 1988-08-04
ATE77388T1 (de) 1992-07-15
ZA88549B (en) 1988-07-27
DK37388A (da) 1988-07-29
ES2042725T3 (es) 1993-12-16
DK37388D0 (da) 1988-01-26
DK169438B1 (da) 1994-10-31
JPS63192800A (ja) 1988-08-10
IE61594B1 (en) 1994-11-16
PT86652A (pt) 1988-02-01
GR3005284T3 (da) 1993-05-24
EP0277002A2 (en) 1988-08-03
DE3871965D1 (de) 1992-07-23
DK196691A (da) 1991-12-05
DE3871965T2 (de) 1993-01-14
DK169840B1 (da) 1995-03-13

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Legal Events

Date Code Title Description
B1 Patent granted (law 1993)
PBP Patent lapsed